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CRA-026440

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Catalog No. T10883Cas No. 847460-34-8

CRA-026440 is a highly potent HDAC inhibitor with inhibitory effects on HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC10 with Ki values of 4,14,11,15,7 and 20 nM, respectively. CRA-026440 has anti-tumor and anti-angiogenic activity and can be used to study colon cancer.

CRA-026440

CRA-026440

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Purity: 96.42%
Catalog No. T10883Cas No. 847460-34-8
CRA-026440 is a highly potent HDAC inhibitor with inhibitory effects on HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC10 with Ki values of 4,14,11,15,7 and 20 nM, respectively. CRA-026440 has anti-tumor and anti-angiogenic activity and can be used to study colon cancer.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$700-In Stock
5 mg$1,800-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:96.42%
Appearance:Solid
Color:Yellow
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Product Introduction

Bioactivity
Description
CRA-026440 is a highly potent HDAC inhibitor with inhibitory effects on HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC10 with Ki values of 4,14,11,15,7 and 20 nM, respectively. CRA-026440 has anti-tumor and anti-angiogenic activity and can be used to study colon cancer.
Targets&IC50
HDAC2:14 nM (ki), HDAC3:11 nM (ki), HDAC6:15 nM (ki), HDAC8:7 nM (ki), HDAC1:4 nM (ki), HDAC10:20 nM (Ki)
In vitro
CRA-026440 exhibits anti-proliferative effects on HUVEC endothelial cells with a GI50 value of 1.41 μM[1].
In tumor cells, treatment with CRA-026440 (0.1-10 μM; 18 hours) leads to the accumulation of acetylated histones and acetylated microtubule proteins, thereby inhibiting tumor cell growth and inducing apoptosis[1].
CRA-026440 (0.1-10 μM; 5 days) inhibits ex vivo angiogenesis in a dose-dependent manner[1].
In vivo
Administered intravenously at a dose of 100 mg/kg daily for three consecutive days, CRA-026440 significantly reduces tumor growth in mice bearing HCT116 or U937 human tumor xenografts[1].
Chemical Properties
Molecular Weight420.46
FormulaC23H24N4O4
Cas No.847460-34-8
SmilesO=C(NO)C1=CC=C(C#CCNC(=O)C2=CC=3C=C(OCCN(C)C)C=CC3N2)C=C1
Relative Density.1.35 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 90 mg/mL (214.05 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3783 mL11.8917 mL23.7835 mL118.9174 mL
5 mM0.4757 mL2.3783 mL4.7567 mL23.7835 mL
10 mM0.2378 mL1.1892 mL2.3783 mL11.8917 mL
20 mM0.1189 mL0.5946 mL1.1892 mL5.9459 mL
50 mM0.0476 mL0.2378 mL0.4757 mL2.3783 mL
100 mM0.0238 mL0.1189 mL0.2378 mL1.1892 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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